Pharmacological studies have demonstrated that the sesquiterpene anisatin is a non-competitive gamma-aminobutyric acid antagonist, being more potent than picrotoxin in this regard. A concise, stereocontrolled total synthesis of anisatin is proposed. The key step in the planned synthesis is an intramolecular thermal cyclization of a monocyclic unsaturated aldehyde to afford the corresponding bicyclic product. Further elaboration of this compound should to lead anisatin.